Trans-resveratrol-loaded nonionic lamellar liquid-crystalline systems: structural, rheological, mechanical, textural, and bioadhesive characterization and evaluation of in vivo anti-inflammatory activity

Int J Nanomedicine. 2017 Sep 14:12:6883-6893. doi: 10.2147/IJN.S138629. eCollection 2017.

Abstract

Resveratrol (Res) is a common phytoalexin present in a few edible materials, such as grape skin, peanuts, and red wine. Evidence has shown the beneficial effects of Res on human health, which may be attributed to its anti-inflammatory activity. However, the poor aqueous solubility of Res limits its therapeutic effectiveness. Therefore, the use of nanostructured delivery systems for Res, such as liquid-crystalline systems, could be beneficial. In this study, we aimed to develop, characterize, and determine the in vivo effectiveness of Res-loaded liquid-crystalline systems. Systems containing copaiba balsam oil, polyethylene glycol-40 hydrogenated castor oil, and water were designed. Results of polarized light microscopy, small-angle X-ray scattering, texture-profile analysis, and flow-rheology analysis showed that the Res-loaded liquid-crystalline system had a lamellar structure, textural and mechanical (hardness, compressibility, and adhesiveness) properties, and behaved as a non-Newtonian fluid, showing pseudoplastic behavior upon skin application. Furthermore, all liquid-crystalline systems presented bioadhesive properties that may have assisted in maintaining the anti-inflammatory activity of Res, since the topical application of the Res-loaded lamellar mesophase liquid crystals resulted in edema inhibition in a carrageenan-induced paw-inflammation mouse model. Therefore, Res-loaded lamellar mesophases represent a promising new therapeutic approach for inhibition of skin inflammation.

Keywords: anti-inflammatory properties; lamellar mesophase; liquid crystals; topical delivery.

MeSH terms

  • Adhesiveness
  • Adhesives / pharmacology*
  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Humans
  • Ions
  • Liquid Crystals / chemistry*
  • Male
  • Materials Testing
  • Mechanical Phenomena*
  • Mice
  • Resveratrol
  • Rheology*
  • Scattering, Small Angle
  • Skin / drug effects
  • Solubility
  • Stilbenes / chemistry*
  • Stilbenes / pharmacology*
  • Sus scrofa
  • X-Ray Diffraction

Substances

  • Adhesives
  • Anti-Inflammatory Agents
  • Ions
  • Stilbenes
  • Resveratrol